Methods for efficacious removal of attached, sucking antropods from human dermis

Abstract

The present invention provides methods of using compositions containing local anesthetic compounds for facilitating the removal of sucking arthropods from the skin of a mammal; for reducing inflammation associated with a bite of a sucking arthropod; for limiting infection from a sucking arthropod; and for enhancing the facilitated removal of sucking arthropods from the skin of a mammal.

What is claimed is: 
     
       1. A method for facilitating removal of attached sucking arthropods from the skin of a mammal comprising topically applying at least one thin layer of a composition for topical application comprising a) 0.05-10% weight/volume of a primary anesthetic having the formula ##STR7## wherein R 1  =H, a C 1-4  alkyl or --COOCH 3  ; R 2  =H or a C 1-4  alkyl;   R 3  =H or CH 3  ;   R 4  =C 1-4  alkyl;   R 5  and R 6  independently=H or C 1-4  alkyl,   where at least one of R 1  and R 2  is C 1-4  alkyl and where at least one of R 5  and R 6  is C 1-4  alkyl, provided that where R 4  and R 5  are joined in R 4  --NR 5  R 6 , R 4  and R 5  together with N form a heterocycloalkyl moiety; or the hydrohalide thereof;     b) a water-soluble carrier which enhances skin permeability; and   c) a compound selected from the group consisting of i) 0.5-20% weight/volume of a secondary anesthetic which is a substituted ester of p-aminobenzoic acid having the formula ##STR8## wherein R 7  =H or Cl; R 8  =C 1-4  alkyl-X, where X=H or --N(R 9 ) 2 , and R 9  =C 1-4  alkyl; or the hydrohalide thereof, and   ii) 0.01-10% weight/volume of an anti-inflammatory compound,   iii) an effective amount of an antibiotic, and   iv) 1-50% weight/volume of an insect repellant; to the sucking arthropod and the immediately surrounding topical area, waiting 5-30 minutes from the application of said at least one thin layer and removing said sucking arthropod.     
     
     
       2. A method for reducing inflammation associated with a sucking arthropod bite comprising topically applying a composition comprising a) 0.05-10% weight/volume of a primary anesthetic having the formula ##STR9## wherein R 1  =H, a C 1-4  alkyl or --COOCH 3  ; R 2  =H or a C 1-4  alkyl;   R 3  =H or CH 3  ;   R 4  =C 1-4  alkyl;   R 5  and R 6  independently=H or C 1-4  alkyl,     where at least one of R 1  and R 2  is C 1-4  alkyl and where at least one of R 5  and R 6  is C 1-4  alkyl, provided that where R 4  and R 5  are joined in R 4  --NR 5  R 6 , R 4  and R 5  together with N form a heterocycloalkyl moiety; or the hydrohalide thereof; b) a water-soluble carrier which enhances skin permeability; and   c) a compound selected from the group consisting of i) 0.5-20% weight/volume of a secondary anesthetic which is a substituted ester of p-aminobenzoic acid having the formula ##STR10## wherein R 7  =H or Cl; R 8  =C 1-4  alkyl-X, where X=H or --N(R 9 ) 2 , and R 9  =C 1-4  alkyl; or the hydrohalide thereof,   ii) 1-50% weight/volume of an insect repellent and   iii) an anti-inflammatory compound selected from the group consisting of one or more of topical astringents; anti-inflammatory steroidal agents; antagonists of prostaglandin; inhibitors of prostaglandin synthetase; antagonist of bradykinin; inhibitors of histamine receptors; and inhibitors of mast cell degranulation to the sucking arthropod and the immediately surrounding topical area as is required to reduce inflammation from said arthropod bite.       
     
     
       3. A method of limiting infection from a sucking arthropod bite comprising topically applying a thin layer of a composition comprising: a) 0.05-10% weight/volume of a primary anesthetic having the formula ##STR11## wherein R 1  =H, a C 1-4  alkyl or --COOCH 3  ; R 2  =H or a C 1-4  alkyl;   R 3  =H or CH 3  ;   R 4  =C 1-4  alkyl;   R 5  and R 6  independently=H or C 1-4  alkyl,   where at least one of R 1  and R 2  is C 1-4  alkyl and where at least one of R 5  and R 6  is C 1-4  alkyl, provided that where R 4  and R 5  are joined in R 4  --NR 5  R 6 , R 4  and R 5  together with N form a heterocycloalkyl moiety; or the hydrohalide thereof;     b) a water-soluble carrier which enhances skin permeability; and   c) a compound selected from the group consisting of i) 0.5-20% weight/volume of a secondary anesthetic which is a substituted ester of p-aminobenzoic acid having the formula ##STR12## wherein R 7  H or Cl; R 8  =C 1-4  alkyl-X, where X=H or --N(R 9 ) 2 , and R 9  =C 1-4  alkyl; or the hydrohalide thereof, and   ii) 1-50% weight/volume of an insect repellent and   iii) an antibiotic selected from the group consisting of one or more of from 100-10,000 unit of bacitracin, polymyxin and nystatin per gram of composition and from 1-10 mg of neomycin gram of composition; one or more times to the sucking arthropod and the immediately surrounding topical area within 48 hours of receiving said bite; making repeated topical applications of said composition in similar thin layers to said areas every 5-30 minutes until said arthropod falls off or becomes easily removable; and making up to five further applications after removal of said arthropod.     
     
     
       4. A method of enhancing the facilitated removal of sucking arthropods by applying a composition for topical application comprising a) 0.05-10% weight/volume of a primary anesthetic having the formula ##STR13## wherein R 1  =H, a C 1-4  alkyl or --COOCH 3  ; R 2  =H or a C 1-4  alkyl;   R 3  =H or CH 3  ;   R 4  =C 1-4  alkyl:   R 5  and R 6  independently=H or C 1-4  alkyl, where at least one of R 1  and R 2  is C 1-4  alkyl and where at least one of R 5  and R 6  is C 1-4  alkyl, provided that where R 4  and R 5  are joined in R 4  --NR 5  R 6 , R 4  and R 5  together with N form a heterocycloalkyl moiety; or the hydrohalide thereof;     b) a water-soluble carrier which enhances skin permeability; and   c) a compound selected from the group consisting of   
     
     
       0. 5-20% weight/volume of a secondary anesthetic which is a substituted ester of p-aminobenzoic acid having the formula ##STR14## wherein R 7  =H or Cl; R 8  =C 1-4  alkyl-X, where X=H or --N(R 9 ) 2 , and R 9  =C 1-4  alkyl; or the hydrohalide thereof, and ii) 0.01-10% weight/volume of an anti-inflammatory compound,   iii) an effective amount of an antibiotic, and   iv) 1-50% weight/volume of N,N'-diethyl-m-toluamide; to the sucking arthropod and the immediately surrounding topical area.   
     
     
       5. A method of using a composition for topical application of arthropod removal comprising a) 0.05-10% weight/volume of a primary anesthetic having the formula ##STR15## wherein R 1  =H, a C 1-4  alkyl or --COOCH 3  ; R 2  =H or a C 1-4  alkyl;   R 3  =H or CH 3  ;   R 4  =C 1-4  alkyl;   R 5  and R 6  independently=H or C 1-4  alkyl, where at least one of R 1  and R 2  is C 1-4  alkyl and where at least one of R 5  and R 6  is C 1-4  alkyl, provided that where R 4  and R 5  are joined in R 4  --NR 5  R 6 , R 4  and R 5  together with N form a heterocycloalkyl moiety; or the hydrohalide thereof;     b) a water-soluble carrier which enhances skin permeability; and   c) a compound selected from the group consisting of i) 0.5-20% weight/volume of a secondary anesthetic which is a substituted ester of p-aminobenzoic acid having the formula ##STR16## wherein R 7  =H or Cl; R 8  =C 1-4  alkyl-X, where X=H or --N(R 9 ) 2 , and R 9  =C 1-4  alkyl; or the hydrohalide thereof, and   ii) 0.01-10% weight/volume of an anti-inflammatory compound,   iii) an effective amount of an antibiotic, and   iv) 1-50% weight/volume of an insect repellent     said method comprising applying said composition to a sucking arthropod attached to human or animal skin and the immediately surrounding topical area, re-applying said composition to said area 7-10 minutes later and then removing said arthropod.